O-Desmethyl gefitinib-d8
Based on 1 Customer Validation
O-Desmethyl gefitinib-d8 is a deuterium labeled O-Desmethyl gefitinib. O-Desmethyl gefitinib is an active metabolite of Gefitinib in human plasma. The formation of O-desmethyl gefitinib is dependent on CYP2D6 activity. O-desmethyl gefitinib inhibits EGFR with an IC50 of 36 nM in subcellular assays.
For research use only. We do not sell to patients.
- Purity : 99.84%
- CAS No.: 2748500-39-0
- Formula: C21H14D8ClFN4O3
- Molecular Weight:440.93
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
IC50: 36 nM (EGFR)[2]
Application
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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CAS No. 2748500-39-0
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Unlabeled CAS 847949-49-9
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Appearance Solid
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Molecular Weight 440.93
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Formula C21H14D8ClFN4O3
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Color White to off-white
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SMILES
OC1=CC2=NC=NC(NC3=CC=C(F)C(Cl)=C3)=C2C=C1OCCCN4C([2H])([2H])C([2H])([2H])OC([2H])([2H])C4([2H])[2H]
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (226.79 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Kobayashi H, et al. Effects of polymorphisms in CYP2D6 and ABC transporters and side effects induced by gefitinib on the pharmacokinetics of the gefitinib metabolite, O-desmethyl gefitinib. Med Oncol. 2016 Jun;33(6):57. [Content Brief]
[2]. McKillop D, et al. Minimal contribution of desmethyl-gefitinib, the major human plasma metabolite of gefitinib, to epidermal growth factor receptor (EGFR)-mediated tumour growth inhibition. Xenobiotica. 2006 Jan;36(1):29-39. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2679 mL | 11.3397 mL | 22.6793 mL | 56.6983 mL |
| 5 mM | 0.4536 mL | 2.2679 mL | 4.5359 mL | 11.3397 mL | |
| 10 mM | 0.2268 mL | 1.1340 mL | 2.2679 mL | 5.6698 mL | |
| 15 mM | 0.1512 mL | 0.7560 mL | 1.5120 mL | 3.7799 mL | |
| 20 mM | 0.1134 mL | 0.5670 mL | 1.1340 mL | 2.8349 mL | |
| 25 mM | 0.0907 mL | 0.4536 mL | 0.9072 mL | 2.2679 mL | |
| 30 mM | 0.0756 mL | 0.3780 mL | 0.7560 mL | 1.8899 mL | |
| 40 mM | 0.0567 mL | 0.2835 mL | 0.5670 mL | 1.4175 mL | |
| 50 mM | 0.0454 mL | 0.2268 mL | 0.4536 mL | 1.1340 mL | |
| 60 mM | 0.0378 mL | 0.1890 mL | 0.3780 mL | 0.9450 mL | |
| 80 mM | 0.0283 mL | 0.1417 mL | 0.2835 mL | 0.7087 mL | |
| 100 mM | 0.0227 mL | 0.1134 mL | 0.2268 mL | 0.5670 mL |
O-Desmethyl gefitinib-d8 Related Classifications
HY-100064S Related Classifications
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